|
rdf:type |
|
|
lifeskim:mentions |
|
|
pubmed:issue |
23
|
|
pubmed:dateCreated |
2006-11-10
|
|
pubmed:abstractText |
Structure-based drug design was exploited in the synthesis of 3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating an alanylamide P4 group with acyclic tertiary amide termini. Optimized hydrophobic contacts of one amide substituent in P4 were complemented by hydrophobicity-modulating features in the second, producing potent fXa inhibitors including examples with excellent anticoagulant properties.
|
|
pubmed:language |
eng
|
|
pubmed:journal |
|
|
pubmed:citationSubset |
IM
|
|
pubmed:chemical |
|
|
pubmed:status |
MEDLINE
|
|
pubmed:month |
Dec
|
|
pubmed:issn |
0960-894X
|
|
pubmed:author |
pubmed-author:BorthwickAlan DAD,
pubmed-author:BrownDavidD,
pubmed-author:Burns-KurtisCynthia LCL,
pubmed-author:CampbellMatthewM,
pubmed-author:ChanChuenC,
pubmed-author:ConveryMáire AMA,
pubmed-author:CroweMiriam CMC,
pubmed-author:DayalSatishS,
pubmed-author:DialloHawaH,
pubmed-author:KellyHenry AHA,
pubmed-author:KingN PaulNP,
pubmed-author:KleanthousSavvasS,
pubmed-author:MasonAndrew MAM,
pubmed-author:MordauntJackie EJE,
pubmed-author:PatelChampaC,
pubmed-author:PatemanAnthony JAJ,
pubmed-author:SengerStefanS,
pubmed-author:ShahGita PGP,
pubmed-author:SmithPaul WPW,
pubmed-author:WatsonNigel SNS,
pubmed-author:WestonHelen EHE,
pubmed-author:YoungRobert JRJ,
pubmed-author:ZhouPingP
|
|
pubmed:issnType |
Print
|
|
pubmed:day |
1
|
|
pubmed:volume |
16
|
|
pubmed:owner |
NLM
|
|
pubmed:authorsComplete |
Y
|
|
pubmed:pagination |
5953-7
|
|
pubmed:meshHeading |
pubmed-meshheading:16982190-Alanine,
pubmed-meshheading:16982190-Amides,
pubmed-meshheading:16982190-Anticoagulants,
pubmed-meshheading:16982190-Antithrombin III,
pubmed-meshheading:16982190-Binding Sites,
pubmed-meshheading:16982190-Crystallography, X-Ray,
pubmed-meshheading:16982190-Drug Design,
pubmed-meshheading:16982190-Factor Xa,
pubmed-meshheading:16982190-Models, Molecular,
pubmed-meshheading:16982190-Molecular Structure,
pubmed-meshheading:16982190-Pyrroles,
pubmed-meshheading:16982190-Structure-Activity Relationship
|
|
pubmed:year |
2006
|
|
pubmed:articleTitle |
Structure- and property-based design of factor Xa inhibitors: pyrrolidin-2-ones with acyclic alanyl amides as P4 motifs.
|
|
pubmed:affiliation |
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Rob.J.Young@gsk.com <Rob.J.Young@gsk.com>
|
|
pubmed:publicationType |
Journal Article
|
